Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/232.8)
  • Patent number: 11339178
    Abstract: Compounds and compositions are provided that comprise selective b-glucuronidase inhibitors. The compounds and compositions can ameliorate the side effects of chemotherapeutic agents and can improve the efficacy of such agents, including irinotecan and non-steroidal anti-inflammatory drugs.
    Type: Grant
    Filed: July 20, 2017
    Date of Patent: May 24, 2022
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Matthew R. Redinbo, Jian Jin, Lindsey James, Sam Pellock, Ranathunga Arachchillage Yamuna Ariyarathna, Stephen Frye
  • Patent number: 11267814
    Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.
    Type: Grant
    Filed: October 30, 2019
    Date of Patent: March 8, 2022
    Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
  • Patent number: 11254651
    Abstract: The present disclosure provides certain compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinpathies such as beta-thalassemia and sickle cell disease. Also provided are pharmaceutical compositions containing such compounds as well as processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: February 22, 2022
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Ming Yu, Zhe Li, Lina Q. Setti
  • Patent number: 11103512
    Abstract: A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: August 31, 2021
    Assignee: Merck Patent GmbH
    Inventors: Michael Lange, Clemens Kuehn, Thomas Fuchss, David Maillard, Marcel Breuning, Marco Poma, Edoardo Burini
  • Patent number: 11065255
    Abstract: A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: July 20, 2021
    Assignee: Merck Patent GmbH
    Inventors: Michael Lange, Clemens Kuehn, Thomas Fuchss, David Maillard, Marcel Breuning, Marco Poma, Edoardo Burini
  • Patent number: 11034663
    Abstract: Disclosed are a tetrahydronaphtho[1,2-b]furan-2(3H)-one derivative of formula (I) and a method of making the same, where definitions of R, R1 and R2 herein are the same as those in the specification. It has been demonstrated by animal experiments that the tetrahydronaphtho[1,2-b]furan-2(3H)-one derivative can significantly inhibit the adjuvant-induced in Wistar male rats so that it can alleviate the primary and secondary lesions, showing a preventive activity to some extent. Therefore, the tetrahydronaphtho[1,2-b]furan-2(3H)-one derivative provided herein is applicable to the preparation of a drug for preventing/treating rheumatoid arthritis, and has promising clinical applications.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: June 15, 2021
    Assignee: SHANGHAI QINGDONG BIOTECHNOLOGY CO., LTD
    Inventors: Qingyan Sun, Weidong Zhang
  • Patent number: 10857122
    Abstract: New uses of hypoestoxide, its derivatives and related compounds for treatment and prevention of neurodegenerative diseases (e.g. Parkinsons disease, Alzheimers disease, Huntingtons disease) are described. More specifically, the invention relates to methods for treating various neurodegenerative diseases through administration of hypoestoxide, its derivatives and related compounds, or a combination thereof to a subject with a neurodegenerative disease such that the symptoms of the disease are treated or at least partially alleviated. Furthermore, the present invention further provides methods of preventing the development of neurodegenerative diseases in individuals who are predisposed to developing a neurodegenerative disease over time.
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: December 8, 2020
    Assignee: IMMUNE MODULATION, INC.
    Inventors: Howard Cottam, Emmanuel Ojo-Amaize, Emeka Nchekwube, Olusola Oyemade
  • Patent number: 10842152
    Abstract: The invention relates to the technical field of the herbicides and/or plant growth regulators. Specifically, the invention primarily relates to novel substituted isothiazolopyridones, and compositions comprising said novel substituted isothiazolopyridones. Further, the present invention relates to processes for the preparation said novel substituted isothiazolopyridones and their use as herbicides and/or plant growth regulators.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: November 24, 2020
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Jullien Rey, Joerg Tiebes, Marc Mosrin, Thomas Droege, Hansjoerg Dietrich, Anu Bheemaiah Machettira, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler, Daniela Portz, Kerstin Ilg, Philippe Rinolfi
  • Patent number: 10822346
    Abstract: Disclosed herein are thienopyrimidine meglumine salts according to Formula (I) used for treating or preventing heart failure:
    Type: Grant
    Filed: April 16, 2019
    Date of Patent: November 3, 2020
    Assignee: CARDURION PHARMACEUTICALS, LLC
    Inventors: Anuj K. Kumar, Raymond E. Forslund
  • Patent number: 10696663
    Abstract: The present invention provides compounds that modulate the interaction of TCR with Nck, compositions thereof, and methods of treatment using the same.
    Type: Grant
    Filed: February 27, 2019
    Date of Patent: June 30, 2020
    Assignee: Artax Biopharma Inc.
    Inventors: Julio Castro, Andrés Gagete Mateos, Peter J. Machin, Christopher Loren VanDeusen
  • Patent number: 10626113
    Abstract: The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: April 21, 2020
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Donald W. Landry, Shixian Deng, Ottavio Arancio, Jole Fiorito, Andrew Wasmuth
  • Patent number: 10590121
    Abstract: Disclosed embodiments concern kinase inhibitors having a structure according to formula 1, such as interleukin receptor associated kinases (IRAK) inhibitors, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent a kinase-associated disease or condition, particularly an IRAK-associated disease or condition.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: March 17, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Vanessa Taylor, Yan Chen, Rose Yen
  • Patent number: 10543176
    Abstract: A topical cream or ointment is provided that provides for the binding to CB1 and/or CB2 receptors for the soothing of dermatological itching. The cream or ointment composition provides the effect of cannabinoids without the actual use of cannabinoids. Several essential oils, including Black Pepper, Ylang Ylang, and Melissa essential oils in combination, contain caryophyllene, a sesquiterpene, in effective amounts to bind to the CB2 receptor and help reduce an urge to itch the skin.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: January 28, 2020
    Inventor: Jessica Kado
  • Patent number: 10463644
    Abstract: The present invention relates to the uses of sesquiterpene lactone compounds and their derivatives in preparing drugs. It belongs to the field of drug technology, specifically relates to the uses of the compounds of Formula (I) in preparing the drugs, especially the uses in preparing the drugs to treat rheumatoid arthritis and treat cancers through inhibiting cancer stem cells.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: November 5, 2019
    Assignees: ACCENDATECH, NANKAI UNIVERSITY
    Inventors: Yue Chen, Quan Zhang, Jing Long, Weiwei Ma, Jiadai Zhai, Xiudong Yang, Hongxia Fan, Yahui Ding, Liang Wang, Bin Han, Xiaoyan Ma, Haoliang Zhang, Chuanjiang Qiu
  • Patent number: 10441577
    Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 15, 2019
    Assignee: HELMHOLTZ ZENTRUM FUER INFEKTIONSFORSCHUNG
    Inventors: Lars Zender, Ramona Rudalska, Daniel Dauch
  • Patent number: 10322128
    Abstract: The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with EGFR inhibitor agents.
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: June 18, 2019
    Assignee: Felicitex Therapeutics, Inc.
    Inventors: Maria Vilenchik, Michael Frid, Alexandra Kuznetsova, Yuriy Gankin, Marc Duey
  • Patent number: 10314843
    Abstract: The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with therapeutic agents that are inhibitors of mitosis (a mitotic inhibitor).
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: June 11, 2019
    Assignee: Felicitex Therapeutics, Inc.
    Inventors: Maria Vilenchik, Michael Frid, Alexandra Kuznetsova, Yuriy Gankin, Marc Duey
  • Patent number: 10106552
    Abstract: Eukaryotic elongation factor 2 kinase inhibitors of the formula where R1, R2, R3a, R3b, R4a, R4b, R5a, R5b, R6a, R6b, R7 and x are as defined in the specification, pharmaceutical compositions and formulations including compounds of the foregoing formula, and methods of preventing, ameliorating or treating indications, conditions, disorders or syndromes associated with elongation factor 2 phosphorylation.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: October 23, 2018
    Assignee: Longevica Pharmaceuticals, Inc.
    Inventor: John H. Dodd
  • Patent number: 9951061
    Abstract: The present invention provides compounds useful as inhibitors of Ca2+/calmodulin-dependent protein kinase (CaMKII), compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: April 24, 2018
    Assignee: Allosteros Therapeutics, Inc.
    Inventors: Daniel E. Levy, Howard Schulman, Bheema Paraselli, Erin Bradley, Sampath K. Nangunoori, Brahmaiah Dabbugoddu, Isabelle Lehoux
  • Patent number: 9783539
    Abstract: Disclosed herein are certain indoloquinolone compounds, methods of preparation thereof, pharmaceutical compositions thereof, and uses thereof, such as their uses as ALK inhibitors.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: October 10, 2017
    Assignee: Jiangsu Ascentage Biomed Development Inc.
    Inventors: Jianyong Chen, Yunlong Zhou, Shaomeng Wang, Ming Guo, Dajun Yang, Lingling Jiao, Yu Jing, Xu Qian, Liu Liu, Longchuan Bai, Chao-Yie Yang, Donna McEachern
  • Patent number: 9745314
    Abstract: Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: August 29, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Angelo Aguilar, Liu Liu, Jianfeng Lu, Donna McEachern
  • Patent number: 9624238
    Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
    Type: Grant
    Filed: May 21, 2014
    Date of Patent: April 18, 2017
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Joseph Barbosa, Kenneth Gordon Carson, Michael Walter Gardyan, Jason Patrick Healy, Qiang Han, Ross Mabon, Praveen Pabba, James Tarver, Jr., Kristen M. Terranova, Ashok Tunoori, Xiaolian Xu
  • Patent number: 9493460
    Abstract: The invention relates to novel compounds which are naphthalene diimides of general formula (I): The compounds are used in therapy, particularly in cancer treatment.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 15, 2016
    Assignee: UCL BUSINESS PLC
    Inventors: Stephen Neidle, Stephan A. Ohnmacht, Mekala Gunaratnam, Aaron Grainger Dale, Marialuisa Micco, Gavin William Collie
  • Patent number: 9388250
    Abstract: Soluble adenylyl cyclase (sAC) is implicated in proliferation of keratinocytes. Inhibitors of sAC are useful for the treatment and/or prevention of psoriasis and other hyperproliferative skin disorders. Assays to identify such compounds are also described.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: July 12, 2016
    Assignee: CORNELL UNIVERSITY
    Inventors: Jochen Buck, Lonny Levin, Jonathan Zippin
  • Patent number: 9365489
    Abstract: The present invention relates to a method for reducing the production of methane emanating from the digestive activities of a ruminant and or for improving ruminant animal performance by using, as active compound at least one nitrooxy alkanoic acid and/or derivative thereof, which is administrated to the animal together with the feed. The invention also relates to the use of these compounds in feed and feed additives such as premix, concentrates and total mixed ration (TMR) or in the form of a bolus.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: June 14, 2016
    Assignee: DSM IP ASSETS B.V.
    Inventors: Stephane Duval, Maik Kindermann
  • Patent number: 9334288
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidase and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplasatic agents or glucuronidase-substrate agents or compounds.
    Type: Grant
    Filed: September 23, 2013
    Date of Patent: May 10, 2016
    Assignee: The University of North Carolina at Chapel Hill
    Inventor: Matthew R. Redinbo
  • Patent number: 9315458
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: April 19, 2016
    Assignee: Takeda Pharmaceutical Company, Limited
    Inventors: Masami Yamada, Shinkichi Suzuki, Takahiro Sugimoto, Minoru Nakamura, Hiroki Sakamoto, Makoto Kamata
  • Patent number: 9284332
    Abstract: Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-fe][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert-Butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-&][1,3]benzo-thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: March 15, 2016
    Assignee: Ambit Biosciences Corporation
    Inventors: Timothy David Gross, Rathan Prasad Achampeta, Janakiram Rao Citineni
  • Patent number: 9283244
    Abstract: Inhibitors of Late SV-40 Factor (LSF) are used to treat cancers such as hepatocellular carcinoma (HCC). In particular, small molecule chemical LSF inhibitors are employed. In addition, the activity and/or pattern of expression of LSF may is used to diagnose cancer, to characterize the cancer (e.g. stage, grade, prognosis, etc.) and also to develop suitable protocols for cancer treatment.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: March 15, 2016
    Assignee: Virginia Commonwealth University
    Inventors: Devanand Sarkar, Paul B. Fisher
  • Patent number: 9238571
    Abstract: The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Robert Ward
  • Patent number: 9238656
    Abstract: This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.
    Type: Grant
    Filed: July 30, 2014
    Date of Patent: January 19, 2016
    Assignee: Cephalon, Inc.
    Inventors: Henry J. Breslin, Matthew A. Curry, Diane E. Gingrich, Keith S. Learn, Gregory R. Ott, Jason C. Wagner
  • Patent number: 9206200
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Patent number: 9198915
    Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: December 1, 2015
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Satish K. Srivastava, Kota V. Ramana
  • Patent number: 9155797
    Abstract: The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: October 13, 2015
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, C. Simone Jude-Fishburn, Guy Lalonde
  • Patent number: 9115133
    Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: August 25, 2015
    Assignee: Advinus Therapeutics Limited
    Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150148314
    Abstract: There are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.
    Type: Application
    Filed: January 27, 2015
    Publication date: May 28, 2015
    Inventors: William Fenical, Paul R. Jensen, James J. La Clair, Lynnie Trzoss, Takashi Fukuda
  • Patent number: 9040528
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20150141418
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Patent number: 9034870
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: May 19, 2015
    Assignees: Purdue Research Foundation, United States Government National Institutes of Health (NIH), U.S. Dept. of Health and Human Services (DHHS), NIH Division of Extramural Inventions and Technology Resources (DEITR)
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell, Yves George Pommier
  • Publication number: 20150133445
    Abstract: The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Mark S. CUSHMAN, Trung X. Nguyen, Martin M. Conda-Sheridan, Yves George Pommier
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Publication number: 20150132352
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150133443
    Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • Patent number: 9029387
    Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 12, 2015
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Publication number: 20150126501
    Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
  • Publication number: 20150126491
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward